Assay Detail
Binding
CHEMBL869835
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Inhibition of [3H]NA uptake at NA transporter expressed in HEK293 cells
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
N-(1,2-diphenylethyl)piperazines: a new class of dual serotonin/noradrenaline reuptake inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.25 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14370 | REBOXETINE | 4.0 | 1 | 7.96 |
| CHEMBL210026 | — | — | 1 | 7.85 |
| CHEMBL386224 | — | — | 1 | 7.80 |
| CHEMBL1175 | DULOXETINE | 4.0 | 1 | 7.72 |
| CHEMBL213287 | — | — | 1 | 7.66 |
| CHEMBL214335 | — | — | 1 | 7.66 |
| CHEMBL213754 | — | — | 1 | 7.51 |
| CHEMBL210027 | — | — | 1 | 7.51 |
| CHEMBL378418 | — | — | 1 | 7.46 |
| CHEMBL375131 | — | — | 1 | 7.42 |
| CHEMBL214237 | — | — | 1 | 7.41 |
| CHEMBL214240 | — | — | 1 | 7.27 |
| CHEMBL379205 | — | — | 1 | 7.21 |
| CHEMBL210126 | — | — | 1 | 7.14 |
| CHEMBL213035 | — | — | 1 | 7.14 |
| CHEMBL210028 | — | — | 1 | 7.05 |
| CHEMBL212763 | — | — | 1 | 6.89 |
| CHEMBL213632 | — | — | 1 | 6.57 |
| CHEMBL386223 | — | — | 1 | 6.52 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 5.28 |
| CHEMBL214273 | — | — | 1 | - |
| CHEMBL209969 | — | — | 1 | - |
| CHEMBL379536 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14370 | REBOXETINE | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL210026 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL386224 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1175 | DULOXETINE | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL213287 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL214335 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL213754 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL210027 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL378418 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL375131 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL214237 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL214240 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL379205 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL210126 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL213035 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL210028 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL212763 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL213632 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL386223 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL41 | FLUOXETINE | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL214273 | — | IC50 | > | 400.0 | nM | - |
| CHEMBL209969 | — | IC50 | > | 400.0 | nM | - |
| CHEMBL379536 | — | IC50 | > | 400.0 | nM | - |